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ADL-5859

产品编号 T6175 CAS 850173-95-4

别名: ADL5859 Hydrochloride, ADL5859 HCl

ADL-5859 (ADL5859 Hydrochloride) 是δ-阿片受体选择性激动剂，Ki 为0.8 nM，对阿片受体 κ 和 μ 具有选择性。

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ADL-5859, CAS 850173-95-4

规格	价格/CNY	货期
1 mg	￥ 378	现货
2 mg	￥ 556	现货
5 mg	￥ 972	现货
10 mg	￥ 1,630	现货
25 mg	￥ 3,220	现货
50 mg	￥ 4,690	现货
100 mg	￥ 6,720	现货
500 mg	￥ 13,500	现货
1 mL * 10 mM (in DMSO)	￥ 1,060	现货

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其他形式的 ADL-5859:

ADL-5859
询价

选择批次

纯度: 99.71%

纯度: 99.11%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	ADL-5859 (ADL5859 Hydrochloride) is a selective δ-opioid receptor agonist ( Ki: 0.8 nM), selectivity against opioid receptor κ, μ, and little inhibition for the hERG channel.
靶点活性	μ opioid receptor:32 nM(Ki), δ opioid receptor:0.8 nM(Ki), κ opioid receptor:37 nM(Ki)
体外活性	ADL5859 agonizes δ-opioid receptor with a 1000-fold selectivity than μ- or κ-opioid receptor with Ki of 32 nM and 37 nM, respectively.ADL5859 displays weak inhibitory activity at the hERG channel with an IC50 of 78 μM. The EC50 of ADL5859 against δ opioid receptor is 20 nM.[1]
体内活性	At the screening dose of 3 mg/kg p.o., ADL5859 produces 100% reversal of hyperalgesia in the inflamed paw. The oral ED50 of ADL5859 in the FCA mechanical hyperalgesia assay is 1.4 mg/kg. The antihyperalgesia produced by ADL5859 (3 mg/kg, p.o.) is reversed by pretreatment with the δ opioid antagonist naltrindole (0.3 mg/kg s.c.), thus demonstrating a δ receptor mediated effect.In the rat forced swim assay, ADL5859 (3 mg/kg p.o.) produces robust antidepressant-like activity, as evidenced by a significant decrease in the time spent immobile and a significant increase in the time spent swimming. The bioavailability of ADL5859 (3 mg/kg p.o.) in rats and dogs is 33% and 66%, respectively.[1]ADL5859 efficiently reduces inflammatory and neuropathic pain mainly by recruiting δ-opioid receptors expressed by peripheral Nav1.8-expressing neurons.[2]
细胞实验	Membrane preparations from Chinese hamster ovary (CHO) cells stably expressing human κ, μ, or δ opioid receptors are prepared. The assay buffer used is composed of 50 mMtris(hydroxymethyl) aminomethaneHCl, pH 7.8, 1.0 mM ethylene glycol bis(β-aminoethyl ether)-N,N,N',N'-tetraacetic acid (EGTA free acid), 5.0 mM MgCl2 10 mg/L leupeptin, 10 mg/L pepstatin A, 200 mg/L bacitracin, and 0.5 mg/L aprotinin. After dilution in assay buffer and homogenization in a Polytron homogenizer for 30 seconds, membrane proteins (10-80 μg) in 250 μL of assay buffer are added to mixtures containing ADL5859 and [3H]diprenorphine (0.5-1.0 nM, 25000-50000 dpm) in 250 μL of assay buffer in 96-well deep-well polystyrene titer plates and incubated at room temperature for 60 minutes. Reactions are terminated by vacuum filtration with a Brandel MPXR-96T harvester through GF/B filters that have been pretreated with a solution of 0.5% polyethylenimine and 0.1% bovine serum albumin for at least 1 hour. The filters arewashed four times with 1.0 mL each of ice-cold 50 mM Tris-HCl, pH 7.8, and 30 μL of Microscint-20 is added to each filter. Radioactivity on the filters is determined by scintillation spectrometry in a Packard TopCount. [3H]Diprenorphine with a specific activity of 50 Ci/mmolisused. The Kd values for [3H]diprenorphine binding are 0.33 nM for the κ and μ receptors and 0.26 nM for the δ receptor. Receptor expression levels, determined as Bmax values from Scatchard analyses, are 4400, 4700, and 2100 fmol/mg of protein for the κ, μ, and δ receptors, respectively. Preliminary experiments are performed to show that no specific binding is lost during the wash of the filters, that binding achieved equilibrium within the incubation time and remained at equilibrium for at least an additional 60 minutes, and that binding is linear with regard to protein concentration. Nonspecific binding, determined in the presence of 10 μM unlabeled naloxone, is less than 10% of total binding.Protein is quantified by the method of Bradford. The data from competition experiments are fit by nonlinear regression analysis with the program Prism using the four-parameter equation for one-site competition, and Ki values are subsequently calculated from EC50 values by the Cheng-Prusoff equation.(Only for Reference)

别名	ADL5859 Hydrochloride, ADL5859 HCl
分子量	428.95
分子式	C24H28N2O3·HCl
CAS No.	850173-95-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: 5 mg/mL (11.65 mM)

DMSO: 80 mg/mL (186.5 mM)

Ethanol: 1 mg/mL (2.33 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
H2O / DMSO / Ethanol	1 mM	2.3313 mL	11.6564 mL	23.3127 mL	58.2819 mL
H2O / DMSO	5 mM	0.4663 mL	2.3313 mL	4.6625 mL	11.6564 mL
H2O / DMSO	10 mM	0.2331 mL	1.1656 mL	2.3313 mL	5.8282 mL
DMSO	20 mM	0.1166 mL	0.5828 mL	1.1656 mL	2.9141 mL
	50 mM	0.0466 mL	0.2331 mL	0.4663 mL	1.1656 mL
	100 mM	0.0233 mL	0.1166 mL	0.2331 mL	0.5828 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Le Bourdonnec B, et al. J Med Chem, 2008, 51(19), 5893-5896. 2. Nozaki C, et al. J Pharmacol Exp Ther, 2012, 342(3), 799-807.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

ADL-5859 850173-95-4 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor inhibit ADL5859 Hydrochloride ADL5859 ADL 5859 Inhibitor ADL5859 HCl ADL 5859 Hydrochloride ADL-5859 Hydrochloride inhibitor

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ADL-5859

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords